Target
Mitogen-activated protein kinase 8
Ligand
BDBM15921
Substrate
biotinylated GST-ATF2
Meas. Tech.
ATF-2 Phosphorylation Assay
pH
7.2±n/a
Temperature
293.15±n/a K
IC50
390±20 nM
Citation
 Zhao, HSerby, MDXin, ZSzczepankiewicz, BGLiu, MKosogof, CLiu, BNelson, LTJohnson, EFWang, SPederson, TGum, RJClampit, JEHaasch, DLAbad-Zapatero, CFry, EHRondinone, CTrevillyan, JMSham, HLLiu, G Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors. J Med Chem 49:4455-8 (2006) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 8
Synonyms:
JNK-46 | JNK1 | JNK1-alpha-1 | MAPK8 | MK08_HUMAN | Mitogen-Activated Protein Kinase 8 (JNK1) | PRKM8 | SAPK1 | SAPK1C | Stress-activated protein kinase JNK1 | c-Jun N-terminal kinase 1 | c-Jun N-terminal kinase 1 (JNK1) | c-Jun N-terminal kinase 1(JNK1) | c-Jun N-terminal kinase 2 (JNK2)
Type:
Enzyme
Mol. Mass.:
48297.57
Organism:
Homo sapiens (Human)
Description:
JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology).
Residue:
427
Sequence:
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR
  
Inhibitor
Name:
BDBM15921
Synonyms:
2-pyridinecarboxamide deriv. 17a | 5-Cyano-6-ethoxy-pyridine-2-carboxylic acid 4-methanesulfonyl-benzylamide | 5-cyano-6-ethoxy-N-[(4-methanesulfonylphenyl)methyl]pyridine-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C17H17N3O4S
Mol. Mass.:
359.4
SMILES:
CCOc1nc(ccc1C#N)C(=O)NCc1ccc(cc1)S(C)(=O)=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated GST-ATF2
Synonyms:
ATF-2-GST | ATF2 | Activating transcription factor 2 | Activating transcription factor 2-GST fusion | GST-ATF2 | biotinylated ATF2 substrate | biotinylated activating transcription factor 2
Type:
Other Protein Type
Mol. Mass.:
12237.77
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
109
Sequence:
MSDDKPFLCTAPGCGQRFTNEDHLAVHKHKHEMTLKFGPARNDSVIVADQTPTPTRFLKNCEEVGLFNELASPFENEFKKASEDDIKKMPLDLSPLATPIIRSKIEEPS